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Anti-cancer medication From Wikipedia, the free encyclopedia
Dabrafenib, sold under the brand name Tafinlar among others, is an anti-cancer medication used for the treatment of cancers associated with a mutated version of the gene BRAF.[2] Dabrafenib acts as an inhibitor of the associated enzyme B-Raf, which plays a role in the regulation of cell growth.
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| Trade names | Tafinlar |
| Other names | GSK-2118436 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a613038 |
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| Routes of administration | By mouth |
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| ECHA InfoCard | 100.215.965 |
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| Formula | C23H20F3N5O2S2 |
| Molar mass | 519.56 g·mol−1 |
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The most common side effects include papilloma (warts), headache, nausea, vomiting, hyperkeratosis (thickening and toughening of the skin), hair loss, rash, joint pain, fever and tiredness.[3] When taken in combination with trametinib, the most common side effects include fever, tiredness, nausea, chills, headache, diarrhea, vomiting, joint pain and rash.[3]
Dabrafenib was approved for medical use in the United States in May 2013,[7] and in the European Union in August 2013.[3]
Dabrafenib is indicated as a single agent for the treatment of people with unresectable or metastatic melanoma with BRAF V600E mutation.[2] Dabrafenib is indicated, in combination with trametinib, for BRAF V600E-positive unresectable or metastatic melanoma, metastatic non-small cell lung cancer, metastatic anaplastic thyroid cancer, and unresectable or metastatic solid tumors.[2][3][8]
Clinical trial data demonstrated that resistance to dabrafenib and other BRAF inhibitors occurs within six to seven months.[9] To overcome this resistance, the BRAF inhibitor dabrafenib was combined with the MEK inhibitor trametinib.[9] In January 2014, the FDA approved this combination of dabrafenib and trametinib for BRAF V600E/K-mutant metastatic melanoma.[10][11] In May 2018, the FDA approved the combination dabrafenib/trametinib as an adjuvant treatment for BRAF V600E-mutated, stage III melanoma after surgical resection based on the results of the COMBI-AD phase 3 study,[12] making it the first oral chemotherapy regimen that prevents cancer relapse for node positive, BRAF-mutated melanoma.[13]
The US Food and Drug Administration (FDA) approved dabrafenib as a single agent treatment for people with BRAF V600E mutation-positive advanced melanoma in May 2013.[7][14]
Dabrafenib was approved for use in the European Union in August 2013.[3]
In April 2017, the European Union approved the combination of dabrafenib with trametinib for BRAF V600-positive advanced or metastatic non small-cell lung cancer (NSCLC).[15][16][3]
In September 2023, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Finlee, intended for the treatment of low- and high-grade glioma (LGG and HGG).[17] The applicant for this medicinal product is Novartis Europharm Limited.[17] Finlee was approved for medical use in the European Union in November 2023.[4]
Dabrafenib is the international nonproprietary name.[18]
Dabrafenib is sold under the brand names Tafinlar[3] and Finlee.[4]
Dabrafenib has clinical activity with a manageable safety profile in clinical trials of phase I and II in patients with BRAF (V600)-mutated metastatic melanoma.[19][20]
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